Ulixertinib (BVD-523, VRT752271)
Molecular Weight(MW): 433.33
Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
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|Description||Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.|
In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM. 
ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay:MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 µL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 µL of substrate solution is added consisting of 16 µM Erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 µl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.
|In vitro||DMSO||86 mg/mL (198.46 mM)|
|Ethanol||15 mg/mL (34.61 mM)|
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